Abstract: The myelocytomatosis viral oncogene homolog (MYC) is one of the most frequently dysregulated driver genes in human cancers. The dysregulation of its expression is closely associated with the occurrence and progression of various tumors. The MYC protein encoded by it mainly functions as a transcription factor and is involved in regulating multiple cellular processes, including cell growth, division, differentiation, metabolism, and apoptosis.Therefore, targeting MYC protein is a potential strategy for tumor treatment. However, due to the lack of a suitable binding pocket in MYC for binding to small-molecule compounds, MYC has long been considered an “undruggable” target. This article outlines the structure and function of MYC, and comprehensively analyzes the currently developed antitumor drugs directly or indirectly targeting MYC, aiming to provide some reference for the development of drugs targeting MYC.